{"title":"Formulation and Evaluation of Flurbiprofen Solid Dispersions using Novel Carriers for Enhancement of Solubility","authors":"Abdullah Khan","doi":"10.22377/AJP.V14I03.3765","DOIUrl":null,"url":null,"abstract":"Introduction: The main objective of the current study is to enhance the solubility and dissolution of poorly water-soluble drug flurbiprofen, a propionic acid derivative, used as non-steroidal anti-inflammatory drug by formulating into solid dispersion (SD) employing various hydrophilic polymers as carriers in the formulation. Materials and Methods: The solubility of drug in various polymers such as AQOAT AS, PVP-K30, hydroxypropryl methyl cellulose, Soluplus, and Kollidon VA 64 was studied. Total 15 SD formulations were prepared by solvent evaporation technique with different polymers and were evaluated for particle size analysis, % practical yield, drug content determination, and in vitro dissolution studies. Results: Based on the evaluation parameters and dissolution studies, SD6 was found to be optimized formulation. The SD6 prepared using flurbiprofen:AQOAT AS:sodium lauryl sulfate as drug:polymer:surfactant in 1:5:2 ratios showed maximum drug release of 99.86 in 15 min when compared with other formulation and the solubility of the formulation SD6 was enhanced 44 folds when compared to that of pure drug. Drug excipient compatibility studies were conducted using FTIR and XRD and scanning electron microscope (SEM) studies were also conducted. FTIR studies showed the compatibility between drug and polymers. XRD and SEM studies showed that the optimized formulation was in amorphous form which fetched in better dissolution of the drug from the SD formulation when compared to the pure drug. Conclusion: This indicates the formulation technology employed with a potential of enhancing bioavailability of poorly water-soluble drug by improving its dissolution rate.","PeriodicalId":8489,"journal":{"name":"Asian Journal of Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":0.4000,"publicationDate":"2020-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"2","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Asian Journal of Pharmaceutics","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.22377/AJP.V14I03.3765","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 2
Abstract
Introduction: The main objective of the current study is to enhance the solubility and dissolution of poorly water-soluble drug flurbiprofen, a propionic acid derivative, used as non-steroidal anti-inflammatory drug by formulating into solid dispersion (SD) employing various hydrophilic polymers as carriers in the formulation. Materials and Methods: The solubility of drug in various polymers such as AQOAT AS, PVP-K30, hydroxypropryl methyl cellulose, Soluplus, and Kollidon VA 64 was studied. Total 15 SD formulations were prepared by solvent evaporation technique with different polymers and were evaluated for particle size analysis, % practical yield, drug content determination, and in vitro dissolution studies. Results: Based on the evaluation parameters and dissolution studies, SD6 was found to be optimized formulation. The SD6 prepared using flurbiprofen:AQOAT AS:sodium lauryl sulfate as drug:polymer:surfactant in 1:5:2 ratios showed maximum drug release of 99.86 in 15 min when compared with other formulation and the solubility of the formulation SD6 was enhanced 44 folds when compared to that of pure drug. Drug excipient compatibility studies were conducted using FTIR and XRD and scanning electron microscope (SEM) studies were also conducted. FTIR studies showed the compatibility between drug and polymers. XRD and SEM studies showed that the optimized formulation was in amorphous form which fetched in better dissolution of the drug from the SD formulation when compared to the pure drug. Conclusion: This indicates the formulation technology employed with a potential of enhancing bioavailability of poorly water-soluble drug by improving its dissolution rate.
引言:本研究的主要目的是通过在制剂中使用各种亲水性聚合物作为载体,将用作非甾体抗炎药的水溶性差的药物氟比洛芬配制成固体分散体(SD),以提高其溶解度和溶出度。材料和方法:研究药物在AQOAT as、PVP-K30、羟丙基甲基纤维素、Soluplus和Kollidon VA 64等聚合物中的溶解度。通过溶剂蒸发技术用不同的聚合物制备了总共15种SD制剂,并对其粒径分析、实际产率%、药物含量测定和体外溶出度研究进行了评估。结果:根据评价参数和溶出度研究,确定SD6为最佳处方。以氟比洛芬:AQOAT AS:十二烷基硫酸钠为原料药:聚合物:表面活性剂,按1∶5∶2的比例制备的SD6与其他制剂相比,在15分钟内的最大药物释放量为99.86,与纯药物相比,SD6的溶解度提高了44倍。使用FTIR和XRD进行了药物-赋形剂相容性研究,还进行了扫描电子显微镜(SEM)研究。FTIR研究显示了药物和聚合物之间的相容性。XRD和SEM研究表明,优化的制剂为无定形形式,与纯药物相比,其使药物从SD制剂中更好地溶解。结论:该制剂技术具有通过提高溶出度来提高难溶性药物生物利用度的潜力。
期刊介绍:
Character of the publications: -Pharmaceutics and Pharmaceutical Technology -Formulation Design and Development -Drug Discovery and Development Interface -Manufacturing Science and Engineering -Pharmacokinetics, Pharmacodynamics, and Drug Metabolism -Clinical Pharmacology, General Medicine and Translational Research -Physical Pharmacy and Biopharmaceutics -Novel Drug delivery system -Biotechnology & Microbiological evaluations -Regulatory Sciences